44 results about "Picoplatin" patented technology

The invention provides a method of treatment of metastatic colorectal cancer by administration of the anti-cancer platinum drug picoplatin in conjunction with cetuximab, 5-FU, and leucovorin in a variety of treatment regimens. The invention also provides a use of picoplatin in conjunction with cetuximab, 5-FU, and leucovorin for treatment of metastatic colorectal cancer. The invention further provides kits adapted for administration of picoplatin in conjunction with cetuximab. Also, methods for determining dosage regimens for patients afflicted with a cancer comprising EGFR are provided.

The present invention provides a method to treat ovarian cancer by the administration of effective amounts of picoplatin and pegylated liposomal doxorubicin.

The invention provides an oral dosage form for the anti-cancer drug picoplatin comprising a core and a coating, the dosage form being free of redox-active metal salts. The core of the tablet is a substantially dry powder comprising about 10 to 60 wt % picoplatin wherein the picoplatin is a particulate of less than about 10 microns average particle diameter, about 40-80 wt % of a filler comprising a substantially water-soluble, water-dispersible, or water-absorbing carbohydrate, and an effective amount of up to about 5 wt % of a lubricant. The dosage form can further include a dispersant.

The invention provides an encapsulated unit dosage form for picoplatin that is adapted for oral administration of the picoplatin containing a substantially dry powder with about 20 to 55 wt % picoplatin in the physical form of a picoplatin particulate wherein an average picoplatin particle diameter is less than about 10 microns. The picoplatin particles are dispersed within the powder of the formulation which includes a substantially water-soluble, water-dispersible, or water-absorbing carbohydrate and an effective amount of up to about 5 wt % of a lubricant.

The invention provides a method of treatment of colorectal cancer by administration of the anti-cancer platinum drug picoplatin in conjunction with 5-FU and leucovorin in a variety of treatment regimens. Dosages, dosing schedules, and ancillary treatments are described.

The invention provides a method of treatment of metastatic hormone-refractory prostate cancer involving substantially as concurrent administration of picoplatin and docetaxel. Prednisone may also be administered. Dosages and dosing regimens are provided.

The invention provides picoplatin, which is a new generation of platinum group metal anti-tumor medicament with steric hinderance effect and is hardly dissolved in pure water, and relates to a preparation formula of the picoplatin (C6H10N2Pt). The injection is prepared by dissolving the picoplatin with mixed solution consisting of polyethylene glycol and solution of hydrochloride sodium chloride in a certain proportion serving as a solvent. The mixed solution obviously improves the dissolvability of the picoplatin up to 15mg / ml; and the injection has easy preparation, stable process and convenient clinical application, and is a perfect picoplatin preparation.

The invention belongs to the field of medicines, and particularly relates to an anti-cancer medicinal composition. The composition comprises arctigenin and a platinum anti-cancer medicament, wherein the platinum medicament is carboplatin, picoplatin or oxaliplatin. Compared with a single medicine, the medicinal composition has a synergistic effect in the aspect of inhibiting non-small cell lung cancers.

The invention provides a method of treatment of colorectal cancer by administration of the anti-cancer platinum drug picoplatin in conjunction with 5-FU and leucovorin in a variety of treatment regimens.

This invention relates to a combination of gemcitabine-[phenyl-(benzoxy-L-alaninyl)]-phosphate (chemical name: 2′-Deoxy-2′,2′-difluoro-D-cytidine-5′-O-[phenyl (benzoxy-L-alaninyl)] phosphate) (NUC-1031) and a platinum-based anticancer agent selected from cisplatin, picoplatin, lipoplatin and triplatin. The combinations are useful in the treatment of cancer, particularly biliary tract and bladder cancer.

The invention relates to a temperature-controlled sustained-release injection containing a platinum compound and a preparation method thereof, the temperature-controlled sustained-release injection comprises effective anti-cancer amount of the platinum compound, an amphiphilic block copolymer and a certain amount of drug release regulator, wherein, the amphiphilic block copolymer is composed of polyethylene glycol and polyester, the mixture of the amphiphilic block copolymer and a solvent without organic solvent has the temperature-sensitive gelatinization feature, which is flowable liquid in the environment that is lower than the body temperature and can be automatically converted to the water-insoluble gel that can not flow and be biodegradable for absorption in an endotherm, and the water-insoluble gel can allow the contained platinum compound to have the local sustained release in a tumor and maintain the effective drug concentration for a plurality of weeks to a plurality of months; the anti-cancer sustained-release gel injection can be injected in the tumor or the tumor periphery or be arranged in the postoperative tumor cavity, thus being used for the treatment of the tumors in different stages. The platinum compound is selected from cisplatin, carboplatin, cycloplatin, eptaplatin, denaplatin, zeniplatin, enloplatin, sulfatodiaminocyclohexane platin, cis-spiroplatin, dexormaplatin, iproplatin, lobaplatin, miboplatin, picoplatin, nedaplatin, ormaplatin, oxaliplatin and so on.

The invention provides a method of treatment of colorectal cancer by administration of the anti-cancer platinum drug picoplatin in conjunction with 5-FU and leucovorin in a variety of treatment regimens.

An anticancer sustained-release gel injection sustained-release microspheres containing platinum-based compound, amphiphilic block copolymer, solvent and release regulator, the mixture of amphiphilic block copolymer and solvent has a temperature sensitive gelatinization characteristic, and can automatically become non-flowing degradable water insoluble gel, which can locally and slowly release drug at tumor foci for several weeks to several months, after injection into body. The adjuvant in the sustained-release microspheres is poly(lactic acid)-glycollic acid copolymer; and the amphiphilic block copolymer is PLGA-PEG-PLGA copolymer. The preparation can be injected into artery, inside a tumor or around a tumor with remarkably reduced systemic toxicity of drug, and can be used for solid tumors at different stages. The platinum-based compound is selected from nedaplatin, carboplatin, cisplatin, enloplatin, ormaplatin, sulfato-1,2-diaminocyclohezane-platinum (SHP), picoplatin, cyclopentylamine platium, zeniplatin, spiroplatin, lobaplatin, iproplatin, oxaliplatin, cycloplatin, and dexormaplatin. The preparation can be used with radioactive particles and can enhance chemotherapy effect.

A anticarcinogenic slow release injection carrying platinum compounds and a synergist thereof is composed of slow release microspheres and a dissolvant, wherein, the slow release microspheres comprise anticancer active components and a slow release adjuvant, and the dissolvant is a special dissolvant containing a suspending agent. The anticancer active component comprises platinum compounds such as sunpla, dicycloplatin, eptaplatin, (cis-amminedichloro(2-methylpyridine) platinum, camphoramine chloroacetic platinum or picoplatin, and the like, and a cytotoxic drug selected from a phosphoinositide 3-kinase inhibitor, pyrimidine analogue and / or a DNA repair enzyme inhibitor; the slow release adjuvant is biocompatible macromolecules such as polylactic acid and copolymer thereof, polyethylene glycol, carboxyl end polylactic acid copolymer, copolymer of dienoic fatty acid and sebacic acid, poly (erucic acid dimer-sebacic acid), poly (fumaric acid-sebacic acid), polifeprosan, polylactic acid, EVAc, and the like, and the suspending agent has the viscosity of 100cp-3,000cp (at the temperature of 20-30 DEG C) and is selected from sodium carboxymethyl cellulose, and the like. The slow release microspheres can also be made into a slow release implant. The slow release injection is injected or placed in tumors or around the tumors, which can improve the curative effects of non-operative therapies such as radiotherapy, chemotherapy, and the like.

The invention discloses a purification method of an anti-tumor drug Picoplatin. The technological process comprises the following steps: dissolving a Picoplatin crude product with an organic solvent at a certain temperature; adding a crystallization solvent into the solution for crystallization at a certain temperature; filtering and drying, so as to obtain a Picoplatin highly-finished product. The purification method of the Picoplatin is simple in operation and comparatively high in yield, the purity of the highly-finished product can reach 99.9% or above, a single impurity can be controlledunder 0.1%, and total impurities can be controlled within 0.2%.

In order to solve the problems of high synthesis difficulty and high cost of potassium trichloroammine platinate in the prior art, the invention discloses a synthesis method of potassium trichloroammine platinate. The method comprises the following steps: by taking chloroplatinous acid or chloroplatinite, ammonium chloride, alkali chloride and carbonate as raw materials, adjusting the pH value of a system to prepare a trichloroammine complexed platinic acid solution, and thenpreparing trichlorine complex potassium platinatefrom the trichlorine complex platinum acid and potassium chloride. According to the synthesis method of the potassium trichloroammine platinate, the required raw materials are simple and easy to obtain, the cost is low, the synthesis conditions are mild, the yield of the potassium trichloroammine platinate is 78% or above, and the potassium trichloroammine platinate can be used as an intermediate for synthesizing anti-cancer drugs such as picoplatin and satraplatin and is suitable for industrial production.

The invention provides formulations for the organoplatinum anticancer drug picoplatin. Self emulsifying compositions, stabilized nanoparticulate compositions, solid dispersions, and nanoparticulate suspensions in oils are provided, along with methods for preparation of the formulations. The formulations can provide improved oral availability of picoplatin relative a to a simple solution of picoplatin such as in water or normal saline solution and can be used in combination therapy.

A method for treatment of small cell lung cancer (SCLC) that does not respond to first-line treatment or that progresses following cessation of first-line organoplatinum chemotherapy is provided that includes the administration of picoplatin, optionally in conjunction with a regimen of best supportive care. Multiple doses of picoplatin can be administered. The picoplatin can also treat SCLC that has metastacized to the brain.

The invention provides an oral dosage form for the anti-cancer drug picoplatin comprising a core and a coating, the dosage form being free of redox-active metal salts. The core of the tablet is a substantially dry powder comprising about 10 to 60 wt% picoplatin wherein the picoplatin is a particulate of less than about 10 microns average particle diameter, about 40-80 wt% of a filler comprising a substantially water-soluble, water-dispersible, or water-absorbing carbohydrate, and an effective amount of up to about 5 wt% of a lubricant. The dosage form can further include a dispersant.

This invention relates to a combination of gemcitabine-[phenyl-(benzoxy-L-alaninyl)]-phosphate (chemical name: 2′-Deoxy-2′,2′-difluoro-D-cytidine-5′-O-[phenyl (benzoxy-L-alaninyl)] phosphate) (NUC-1031) and a platinum-based anticancer agent selected from cisplatin, picoplatin, lipoplatin and triplatin. The combinations are useful in the treatment of cancer, particularly biliary tract and bladder cancer.

The invention provides an oral dosage form for the anti-cancer drug picoplatin comprising a core and a coating, the dosage form being free of redox-active metal salts. The core of the tablet is a substantially dry powder comprising about 10 to 60 wt% picoplatin wherein the picoplatin is a particulate of less than about 10 microns average particle diameter, about 40-80 wt% of a filler comprising asubstantially water-soluble, water-dispersible, or water-absorbing carbohydrate, and an effective amount of up to about 5 wt% of a lubricant. The dosage form can further include a dispersant.

The invention provides a method of treatment of colorectal cancer by administration of the anti-cancer platinum drug picoplatin in conjunction with 5-FU and leucovorin in a variety of treatment regimens. Dosages, dosing schedules, and ancillary treatments are described.

The invention relates to a method for detecting an antitumor medicine, namely a picoplatin bulk medicine and impurities thereof. The method comprises the following specific steps of: 1, adopting high performance liquid chromatography, wherein the chromatographic conditions are that: octadecylsilane chemically bonded silica is used as filler; a flowing phase is a mixed solution of a buffer salt solution (pH is 4.0 to 6.0) of ocane sulfonic acid sodium, sodium heptanesulfonate or monopotassium phosphate and acetonitrile or methanol; the detection wavelength is 200 to 260nm; the column temperature is 25 to 45 DEG C; the flow speed of the flowing phase is 0.5 to 2.0ml / min; 2, preparing a sample solution, namely preparing a 0.1 to 0.3mg / ml solution containing picoplatin by using pure water or normal saline, and keeping in a dark place; and 3, determining, namely injecting 5 to 20 mu L of the sample solution into a high performance liquid chromatograph, recording a chromatogram and analyzing. By the method, the picoplatin can be detected, and the impurities in the picoplatin bulk medicine can be detected easily, quickly and flexibly.

The invention relates to a novel method for preparing picoplatin. The technical scheme adopts following steps of: firstly generating potassium tetraiodoplatinate by reacting potassium tetrachloro platinum with potassium iodide to improve the activity of reactants; generating triiodo (2-picoline) platinum (II) potassium by reacting the potassium tetraiodoplatinate with 2- picoline; generating Cis-2 iodine-ammonia and (2-picoline) platinum (II) by reacting triiodo (2-picoline) platinum (II) potassium with ammonia water; adding the Cis-2 iodine-ammonia and the (2-picoline) platinum (II) together to deionized water; stirring the deionized water for reaction at the room temperature; filtering silver iodide precipitate when the reaction is completed; and adding potassium chloride so as to gradually separate out crystallized products of the picoplatin. In the invention, the reaction is more complete, the utilization of the platinum and the yield are enhanced, the products do not have silver irons, and the problem that the silver irons are exceeded needs not to be worried.

The invention provides picoplatin, which is a new generation of platinum group metal anti-tumor medicament with steric hinderance effect and is hardly dissolved in pure water, and relates to a preparation formula of the picoplatin (C6H10N2Pt). The injection is prepared by dissolving the picoplatin with mixed solution consisting of polyethylene glycol and solution of hydrochloride sodium chloride in a certain proportion serving as a solvent. The mixed solution obviously improves the dissolvability of the picoplatin up to 15mg / ml; and the injection has easy preparation, stable process and convenient clinical application, and is a perfect picoplatin preparation.